CA2748218C - Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof - Google Patents

Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof Download PDF

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Publication number
CA2748218C
CA2748218C CA2748218A CA2748218A CA2748218C CA 2748218 C CA2748218 C CA 2748218C CA 2748218 A CA2748218 A CA 2748218A CA 2748218 A CA2748218 A CA 2748218A CA 2748218 C CA2748218 C CA 2748218C
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Prior art keywords
pyrazol
pyridazin
pyrimidin
morpholin
ethoxy
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CA2748218A
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English (en)
French (fr)
Other versions
CA2748218A1 (en
Inventor
Axel Becker
Clemens Kuehn
Christoph Saal
Oliver Schadt
Dieter Dorsch
Eva Kriegbaum
Frank Stieber
Cristina Donini
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Merck Patent GmbH
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Merck Patent GmbH
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08Bridged systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
CA2748218A 2008-12-22 2009-11-24 Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof Active CA2748218C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08022253.2 2008-12-22
EP08022253 2008-12-22
PCT/EP2009/008358 WO2010072295A1 (en) 2008-12-22 2009-11-24 Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof

Publications (2)

Publication Number Publication Date
CA2748218A1 CA2748218A1 (en) 2010-07-01
CA2748218C true CA2748218C (en) 2017-08-29

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ID=41609799

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CA2748218A Active CA2748218C (en) 2008-12-22 2009-11-24 Novel polymorphic forms of 6-(1-methyl-1h-pyrazol-4-yl)-2-{3-[5-(2-morpholin-4-yl-ethoxy)-pyrimidin-2-yl]-benzyl}-2h-pyridazin-3-one dihydrogenphosphate and processes of manufacturing thereof

Country Status (32)

Country Link
US (1) US8586599B2 (sl)
EP (1) EP2361250B1 (sl)
JP (2) JP5690741B2 (sl)
KR (1) KR101663335B1 (sl)
CN (1) CN102264729B (sl)
AR (1) AR074686A1 (sl)
AU (1) AU2009331990B2 (sl)
BR (1) BRPI0923480B8 (sl)
CA (1) CA2748218C (sl)
CL (1) CL2011001278A1 (sl)
CO (1) CO6331435A2 (sl)
CY (1) CY1114659T1 (sl)
DK (1) DK2361250T3 (sl)
EA (1) EA019320B1 (sl)
EC (1) ECSP11011219A (sl)
ES (1) ES2434247T3 (sl)
HK (1) HK1164837A1 (sl)
HR (1) HRP20130993T1 (sl)
IL (1) IL213647A (sl)
MX (1) MX2011006682A (sl)
MY (1) MY160526A (sl)
NZ (1) NZ594172A (sl)
PE (1) PE20120016A1 (sl)
PL (1) PL2361250T3 (sl)
PT (1) PT2361250E (sl)
SG (1) SG172128A1 (sl)
SI (1) SI2361250T1 (sl)
SM (1) SMT201300133B (sl)
TW (1) TWI448463B (sl)
UA (1) UA103646C2 (sl)
WO (1) WO2010072295A1 (sl)
ZA (1) ZA201105394B (sl)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102008062826A1 (de) * 2008-12-23 2010-07-01 Merck Patent Gmbh Pyridazinonderivate
KR20180092096A (ko) * 2017-02-08 2018-08-17 에이비온 주식회사 트리아졸로 피라진 유도체의 신규한 다형체 및 이의 제조 방법
EP3697776B1 (en) 2017-10-17 2023-04-19 Palau Pharma, S.L.U. Synthesis of 4-aminopyrimidine compounds

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Publication number Publication date
CO6331435A2 (es) 2011-10-20
CY1114659T1 (el) 2016-10-05
BRPI0923480B1 (pt) 2020-10-13
PL2361250T3 (pl) 2014-01-31
SI2361250T1 (sl) 2013-12-31
CL2011001278A1 (es) 2011-09-30
CA2748218A1 (en) 2010-07-01
TWI448463B (zh) 2014-08-11
PE20120016A1 (es) 2012-01-24
HK1164837A1 (en) 2012-09-28
KR101663335B1 (ko) 2016-10-06
HRP20130993T1 (hr) 2013-11-22
AU2009331990B2 (en) 2016-04-14
WO2010072295A1 (en) 2010-07-01
EP2361250B1 (en) 2013-08-07
SMT201300133B (it) 2014-03-07
JP2012513417A (ja) 2012-06-14
IL213647A (en) 2013-11-28
TW201028409A (en) 2010-08-01
US20110257180A1 (en) 2011-10-20
US8586599B2 (en) 2013-11-19
AR074686A1 (es) 2011-02-02
MX2011006682A (es) 2011-07-13
JP5860125B2 (ja) 2016-02-16
EP2361250A1 (en) 2011-08-31
UA103646C2 (ru) 2013-11-11
DK2361250T3 (da) 2013-11-04
KR20110089462A (ko) 2011-08-08
PT2361250E (pt) 2013-11-11
NZ594172A (en) 2013-04-26
MY160526A (en) 2017-03-15
CN102264729B (zh) 2014-03-05
ZA201105394B (en) 2012-03-28
BRPI0923480A2 (pt) 2016-08-09
BRPI0923480B8 (pt) 2021-05-25
AU2009331990A1 (en) 2011-08-11
EA019320B1 (ru) 2014-02-28
ECSP11011219A (es) 2011-12-30
CN102264729A (zh) 2011-11-30
JP5690741B2 (ja) 2015-03-25
ES2434247T3 (es) 2013-12-16
IL213647A0 (en) 2011-07-31
SG172128A1 (en) 2011-07-28
JP2015028093A (ja) 2015-02-12
EA201100973A1 (ru) 2012-01-30

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